HM43239 is an orally active small molecule inhibitor of FLT3 that selectively inhibits not only FLT3 wild type, ITD mutants or TKD mutations, but also FLT3 ITD/TKD double mutations. HM43239 directly inhibits the kinase activity of FLT3 as a reversible Type I inhibitor and effectively modulates downstream p-STAT5 and p-ERK. HM43239 also demonstrated inhibition of SYK, JAK1/2 and TAK1, known to be involved in tumor cell proliferation and/or differentiation HM43239 monotherapy induced dose-dependent regression of tumor growth in FLT3 wild-type and FLT3 mutated leukemia cancer cell line.
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名称 | HM43239 |
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Iupac 化学名称 | rel-5-Chloro-N-[3-cyclopropyl-5-[[(3R,5S)-3,5-dimethyl-1-piperazinyl]methyl]phenyl]-4-(6-methyl-1H-indol-3-yl)-2-pyrimidinamine |
同义词 | HM43239; HM-43239; HM 43239; Tuspetinib |
英文同义词 | HM43239; HM-43239; HM 43239; Tuspetinib |
分子式 | C29H33ClN6 |
分子量 | 501.07 |
Smile | CC1=CC2=C(C=C1)C(C3=NC(NC4=CC(CN5C[C@@H](C)N[C@@H](C)C5)=CC(C6CC6)=C4)=NC=C3Cl)=CN2 |
InChiKey | FZLSDZZNPXXBBB-KDURUIRLSA-N |
InChi | InChI=1S/C29H33ClN6/c1-17-4-7-24-25(12-31-27(24)8-17)28-26(30)13-32-29(35-28)34-23-10-20(9-22(11-23)21-5-6-21)16-36-14-18(2)33-19(3)15-36/h4,7-13,18-19,21,31,33H,5-6,14-16H2,1-3H3,(H,32,34,35)/t18-,19+ |
Cas号 | 2569527-64-4 |
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包装 | 价格 | 库存 | 纯度 | 备货期 |
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大货 | 询价 | 询价 | 询价 |
外观性状 | 固体粉末 |
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纯度 | 98% Min. |
存储 | 短期(几天到几周)为0-4摄氏度,长期(几个月)为-20摄氏度 |
可溶性 | 溶于DMSO |
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运输条件 | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周. |
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Mechanism | |
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Clinical study |
1. Kim J, Bae I, Choi J, Kim M, Byun J, Moon M, Lee E, Kim Y, Kang H, Kim E, Jung S, Ahn Y, Kim Y, Suh K. Abstract 1293: HM43239, a novel FLT3 inhibitor in overcoming resistance for acute myeloid leukemia. Cancer Res. 2019 July 1;79(13_Supplement):1293. doi: 10.1158/1538-7445.AM2019-1293.
2. Lee M, Young E, Moon M, Byun J, Yu H, Kang S, Lee J, Lee K, Kim E, Lee H, Kim Y, Ahn Y, Suh K, Kim S. Abstract 804: Antitumor activity of the potent and novel FLT3 inhibitor HM43239 in acute myeloid leukemia. Cancer Res. 2018 July 1;78(13_Supplement):804. doi: 10.1158/1538-7445.AM2018-804.